| 产品描述: | Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo |
| 靶点: |
5-HT1A Receptor:1.5 nM (Ki);5-HT2A Receptor:2.5 nM (Ki);5-HT2B Receptor:0.19 nM (Ki);5-HT7 Receptor:2.7 nM (Ki);D2 Receptor;D3 Receptor;D4 Receptor;DopamineReceptor; 5-HTReceptor |
| 体内研究: |
Brilaroxazine (oral gavage; 10 mg/kg; twice daily; 28 days) limits the functional and structural effects of pulmonary arterial hypertension (PAH), with significant improvements in pulmonary hemodynamics, right ventricular (RV) hypertrophy, SO2, and pulmonary blood vessel structural changes. Animal Model: SD-rats Dosage: 10 mg/kg Administration: Oral gavage; twice daily; 28 days Result: Had the efficacy in PAH, and mitigated the functional and structural effects of MCT-induced PAH. |
| 参考文献: |
1. Reviva Pharmaceuticals Reports RP5063 Positive Efficacy Results for Memory Deficits 2. Bhat L, et al. Evaluation of the effects of RP5063, a novel, multimodal, serotonin receptor modulator, as single-agent therapy and co-administrated with sildenafil, bosentan, and treprostinil in a monocrotaline-induced pulmonary arterial hypertension rat 3. L. Bhat,et al. Rp5063 Prevents Monocrotaline Induced Pulmonary Arterial Hypertension In Rats. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.22 ml |
11.102 ml |
22.204 ml |
| 5 mM |
0.444 ml |
2.22 ml |
4.441 ml |
| 10 mM |
0.222 ml |
1.11 ml |
2.22 ml |
| 50 mM |
0.044 ml |
0.222 ml |
0.444 ml |
|
| 注意: |
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